ATE454395T1 - ESTROGEN DERIVATIVES AS STEROID SULPHATASE INHIBITORS - Google Patents

ESTROGEN DERIVATIVES AS STEROID SULPHATASE INHIBITORS

Info

Publication number
ATE454395T1
ATE454395T1 AT04713124T AT04713124T ATE454395T1 AT E454395 T1 ATE454395 T1 AT E454395T1 AT 04713124 T AT04713124 T AT 04713124T AT 04713124 T AT04713124 T AT 04713124T AT E454395 T1 ATE454395 T1 AT E454395T1
Authority
AT
Austria
Prior art keywords
group
steroid sulphatase
ring system
estrogen derivatives
sulphatase inhibitors
Prior art date
Application number
AT04713124T
Other languages
German (de)
Inventor
Mathew Leese
Alan Purohit
Michael John Reed
Simon Paul Newman
Surinder K Chander
Fabrice Jourdan
Barry V L Potter
Original Assignee
Sterix Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GB0306717A external-priority patent/GB0306717D0/en
Priority claimed from GB0315885A external-priority patent/GB0315885D0/en
Application filed by Sterix Ltd filed Critical Sterix Ltd
Application granted granted Critical
Publication of ATE454395T1 publication Critical patent/ATE454395T1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Molecular Biology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

The present invention provides a compound comprising a steroidal ring system and an optional group R1 selected from any one of —OH, a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group; wherein the D ring of the steroidal ring system is substituted by a group R2 of the formula -L-R3, wherein L is an optional linker group and R3 is selected from groups which are or which comprise one of a nitrite group, an alcohol, an ester, an ether, an amine and an alkene, provided that when R3 is or comprises an alcohol, L is present; and wherein the A ring of the steroidal ring system is substituted at position 2 or 4 with a group R4, wherein R4 is a hydrocarbyl group.
AT04713124T 2003-03-24 2004-02-20 ESTROGEN DERIVATIVES AS STEROID SULPHATASE INHIBITORS ATE454395T1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB0306717A GB0306717D0 (en) 2003-03-24 2003-03-24 Compound
GB0315885A GB0315885D0 (en) 2003-07-07 2003-07-07 Compound
PCT/GB2004/000705 WO2004085459A1 (en) 2003-03-24 2004-02-20 Oestrogen derivatives as inhibitors of steroid sulphatase

Publications (1)

Publication Number Publication Date
ATE454395T1 true ATE454395T1 (en) 2010-01-15

Family

ID=33099976

Family Applications (1)

Application Number Title Priority Date Filing Date
AT04713124T ATE454395T1 (en) 2003-03-24 2004-02-20 ESTROGEN DERIVATIVES AS STEROID SULPHATASE INHIBITORS

Country Status (15)

Country Link
US (1) US7893284B2 (en)
EP (1) EP1608671B1 (en)
JP (1) JP4719144B2 (en)
AT (1) ATE454395T1 (en)
AU (1) AU2004224053B2 (en)
BR (1) BRPI0408703A (en)
CA (1) CA2520142C (en)
DE (1) DE602004024966D1 (en)
DK (1) DK1608671T3 (en)
EA (1) EA011123B1 (en)
ES (1) ES2339450T3 (en)
HK (1) HK1082258A1 (en)
MX (1) MXPA05010339A (en)
PL (1) PL378577A1 (en)
WO (1) WO2004085459A1 (en)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0113920D0 (en) 2001-06-07 2001-08-01 Sterix Ltd Composition
US8030298B2 (en) 2005-05-26 2011-10-04 Abbott Products Gmbh 17β-HSD1 and STS inhibitors
US8288367B2 (en) 2006-11-30 2012-10-16 Solvay Pharmaceuticals Gmbh Substituted estratriene derivatives as 17BETA HSD inhibitors
WO2008090517A2 (en) * 2007-01-26 2008-07-31 Piramal Life Sciences Limited Enriched plant extract, compound, and methods for the treatment of proliferative disorders
EP2149371A1 (en) 2008-07-28 2010-02-03 PregLem S.A. Use of steroid sulfatase inhibitors for the treatment of preterm labor
WO2010024930A2 (en) 2008-08-28 2010-03-04 President And Fellows Of Harvard College Cortistatin analogues and syntheses therof
JP2012524778A (en) * 2009-04-22 2012-10-18 プレジデント アンド フェロウズ オブ ハーバード カレッジ Angiogenesis inhibitor
WO2012116290A2 (en) * 2011-02-25 2012-08-30 Washington University Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
EP3572417A3 (en) 2011-10-14 2020-03-25 Sage Therapeutics, Inc. 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
MX365644B (en) 2012-12-18 2019-06-10 Univ Washington Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same.
US9512170B2 (en) 2013-03-01 2016-12-06 Washington University Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
US9365502B2 (en) 2013-03-11 2016-06-14 Washington University Neuroactive substituted cyclopenta[b]phenanthrenes as modulators for GABA type-A receptors
US9562026B2 (en) 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
RU2700264C2 (en) 2013-04-17 2019-09-16 Сейдж Терапьютикс, Инк. 19-nor neuroactive steroids and methods of using them
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
KR102239541B1 (en) 2013-04-17 2021-04-14 세이지 테라퓨틱스, 인크. 19-nor c3,3-disubstituted c21-n-pyrazolyl steroids and methods of use thereof
WO2014169831A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof
EP3868382A1 (en) 2013-07-19 2021-08-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
LT3488852T (en) 2013-08-23 2021-02-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
EA201891279A1 (en) 2013-12-24 2019-01-31 Президент Энд Феллоус Оф Гарвард Колледж ANALOGUES OF CORTISTATIN, THEIR SYNTHESIS AND APPLICATIONS
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
BR112017007902B1 (en) 2014-10-16 2023-12-05 Sage Therapeutics, Inc COMPOUND AND ITS SALT, PHARMACEUTICAL COMPOSITION AND USE OF SAID COMPOUND AND ITS SALT IN THE MANUFACTURE OF A MEDICINE FOR THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM
LT3206493T (en) 2014-10-16 2020-08-25 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
SI3224269T1 (en) 2014-11-27 2020-10-30 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
ES2857082T3 (en) 2015-01-26 2021-09-28 Sage Therapeutics Inc Compositions and methods for the treatment of CNS disorders
JP6875996B2 (en) 2015-02-20 2021-05-26 セージ セラピューティクス， インコーポレイテッド Neurostimulatory steroids, compositions, and their use
EP3294298A4 (en) 2015-05-08 2018-10-17 President and Fellows of Harvard College Cortistatin analogues, syntheses, and uses thereof
WO2017004411A1 (en) 2015-07-01 2017-01-05 President And Fellows Of Harvard College Cortistatin analogues and syntheses and uses thereof
BR112018075406A2 (en) * 2016-06-15 2019-03-19 Sony Corp information processing apparatus, observation system, observation method, and program.
DK3481844T3 (en) 2016-07-11 2024-07-22 Sage Therapeutics Inc C7, C12 and C16 substituted neuroactive steroids and their methods of use
MA45599A (en) 2016-07-11 2019-05-15 Sage Therapeutics Inc NEUROACTIVE STEROIDS SUBSTITUTED FOR C17, C20 AND C21 AND THEIR USE PROCEDURES
WO2020243488A1 (en) 2019-05-31 2020-12-03 Sage Therapeutics, Inc. Neuroactive steroids and compositions thereof

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4994439A (en) * 1989-01-19 1991-02-19 California Biotechnology Inc. Transmembrane formulations for drug administration
DE19723794A1 (en) * 1997-06-06 1998-12-10 Jenapharm Gmbh Non-estrogenic derivatives of estradiol with antioxidant activity
US6288050B1 (en) * 1997-07-18 2001-09-11 Duquesne University Of The Holy Ghost Steroid sulfatase inhibitors and methods for making and using the same
GB2331987B (en) * 1997-12-04 2002-11-27 Imperial College Polycyclic sulphamate inhibitors of oestrone sulphatase
US6046186A (en) * 1997-12-24 2000-04-04 Sri International Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use
CA2334119C (en) * 1998-06-10 2011-09-13 Sterix Limited Pharmaceutical composition with tumor necrosis factor a and 2-methoxyestrone-3-o-sulphamate for inhibition of estrone sulphatase
EP1173182A2 (en) * 1999-04-30 2002-01-23 Sterix Limited Use of estrone derivatives as antitumour agents
JPWO2001081364A1 (en) * 2000-04-24 2004-01-08 協和醗酵工業株式会社 Estra-1,3,5 (10) -triene derivative
ES2247102T3 (en) * 2000-05-11 2006-03-01 Research Institute For Medicine And Chemistry Inc. COLA DERIVATIVES-1,3,5 (10) -TRIENO AND PREGNA-1,3,5 (10) -TRIEN 2-SUBSTITUTES AND ITS BIOLOGICAL ACTIVITY.
JP2004517045A (en) * 2000-08-18 2004-06-10 ザ ボード オブ トラスティーズ オブ ザ ユニバーシティ オブ イリノイ Prodrugs of betulinic acid derivatives for treatment of cancer and HIV
GB0020498D0 (en) * 2000-08-18 2000-10-11 Sterix Ltd Compound
WO2002062347A1 (en) 2001-02-05 2002-08-15 Oncology Sciences Corporation Method and composition of novel compounds for the therapy and targeting of the primary modalities of cancer cell proliferation and homeostasis
GB0421106D0 (en) * 2004-09-22 2004-10-27 Sterix Ltd Compound

Also Published As

Publication number Publication date
ES2339450T3 (en) 2010-05-20
CA2520142A1 (en) 2004-10-07
US20060094696A1 (en) 2006-05-04
WO2004085459A1 (en) 2004-10-07
EA011123B1 (en) 2008-12-30
JP2006521335A (en) 2006-09-21
AU2004224053B2 (en) 2011-06-09
CA2520142C (en) 2011-01-04
JP4719144B2 (en) 2011-07-06
DE602004024966D1 (en) 2010-02-25
MXPA05010339A (en) 2005-12-14
PL378577A1 (en) 2006-05-02
EA200501426A1 (en) 2006-06-30
BRPI0408703A (en) 2006-03-07
US7893284B2 (en) 2011-02-22
EP1608671A1 (en) 2005-12-28
DK1608671T3 (en) 2010-05-10
AU2004224053A1 (en) 2004-10-07
EP1608671B1 (en) 2010-01-06
HK1082258A1 (en) 2006-06-02

Similar Documents

Publication Publication Date Title
ATE454395T1 (en) ESTROGEN DERIVATIVES AS STEROID SULPHATASE INHIBITORS
DOP2011000301A (en) DERIVATIVES OF AZAADAMANTANO AND METHODS OF USE OF THE SAME
CO6150144A2 (en) INHIBITORS OF HUMAN TYPHOSINE PHOSPHATASE PROTEIN AND METHODS OF USE
GT200100007A (en) ANTIGONISTS OF THE CORTICOTROPINE RELEASE FACTOR.
HUP0002976A2 (en) Hard surface cleaning composition
ES2185338T3 (en) DERIVATIVES OF FUMAGILOL AND PROCEDURES FOR ITS MANUFACTURE.
RS52931B (en) Viral polymerase inhibitors
ATE303399T1 (en) STEROIDS AS AGONISTS FOR FXR
TR200101906T2 (en) Quinolinecarboxamides as antiviral agents
CR9375A (en) CYCLOPROPANOCARBOXAMIDE DERIVATIVES
AR006390A1 (en) LACTAMA DERIVATIVES
AR067613A1 (en) PK-DNA INHIBITORS, USE AND SYNTHESIS OF THE SAME
DE60032440D1 (en) Holder for the combustion chamber of a gas turbine
DK1311619T3 (en) Use of a bitumen / wax composition
ATE451159T1 (en) DEFOAMERS FOR AQUEOUS SYSTEMS
ES2175989T3 (en) DERIVED FROM TESTOSTERONE.
ATE411287T1 (en) NEW METALPROTEINASE INHIBITORS
WO2006032885A3 (en) 2-substituted estrogen sulphamates for inhibition of steroid sulphatase
AR064306A1 (en) ANGIOTENSIN II RECEIVER ANTAGONISTS
DK1051177T3 (en) Steroidal 3-O-Sulfamate derivatives as inhibitors of oestrone sulfatase
ATE218060T1 (en) COMPOSITIONS THAT PREVENT BETA-AMYLOID PROTEIN RELATED CYTOTOXICITY
AR028743A1 (en) DERIVATIVES OF N-TRIAZOLILMETIL-PIPERAZINA WITH ANTAGONIST ACTION OF NEUROQUININE RECEPTORS
DE69913705D1 (en) NEW COFACTORS FOR METHYL TRANSFERASES
MX2008011292A (en) Steroidal compounds as steroid sulphatase inhibitors.
DK1255745T3 (en) Synthesis of water-soluble 9-dihydro-paclitaxel derivatives from 9-dihydro-13-acetylbaccatin III

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties